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Biochem J. 2012 Dec 15;448(3):417-23. doi: 10.1042/BJ20121513.

Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.

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  • 1Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.

Abstract

Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signalling in cancer, are thought to bind only the active conformation of the EGFR-TKD (tyrosine kinase domain). Through parallel computational and crystallographic studies, we show in the present study that erlotinib also binds the inactive EGFR-TKD conformation, which may have significant implications for its use in EGFR-mutated cancers.

PMID:
23101586
[PubMed - indexed for MEDLINE]
PMCID:
PMC3507260
Free PMC Article
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